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[바이오클론] [APExBIO한국독점대리점] Linezolid (CAS# 165800-03-3) "A5181"
제품(기술)분류: 시약 > Chemical Reagent
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Linezolid

Cat# A5181

CAS# 165800-03-3

 

  Background  

Linezolid, a synthetic oxazolidinone antimicrobial, shows a wide spectrum against Gram-positive bacteria andmultidrug-resistant bacteria such as anaerobes, methicillin-resistant Staphylococcus aureus (MRSA), vancomycin-resistant enterococci, penicillin-resistant pneumococci and streptococcus [1,2].

Oxazolidinones could inhibit protein synthesis by binding to a site on the bacterial 23S ribosomal RNA of the 50S subunit and prevent the formation of a functional 70S-initiation complex. Linezolid is also a weak, nonselective and reversible inhibitor of monoamine oxidase [2].

In Vitro: Linezolid was a potent inhibitor of cell-free transcription-translation in E. coli. IC50 was 1.8 mM[3]. linezolid MICs vary slightly owing to the different test method and laboratory. The MIC values were between 0.5 and 4 mg/L for streptococci, enterococci and staphylococci [4].

Clinical Trials: Linezolid is fully bioavailable following oral administration, with maximum plasma linezolid concentrations achieved between 1 and 2 hours after oral administration. The elimination half-life of linezolid is 5–7 hours, and twice-daily administration of 400–600mg provides steady-state concentrations in the therapeutic range[5].

In clinical trials involving hospitalised patients with skin/soft tissue infections (predominantly S. aureus), intravenous/oral administration of linezolid (up to 1250 mg/day) produced clinical success in > 83% of individuals. In patients with community-acquired pneumonia, success rates were > 94%[6]. Linezolid could also be used in patients with nosocomial pneumonia[7].Linezolid appears to be well tolerated and the most common side effects is gastrointestinal disturbances [6].

 

  Chemical Properties  

Physical Appearance A solid
Storage Store at -20°C
M.Wt 337.35
Cas No. 165800-03-3
Formula C16H20FN3O4
Solubility ≥16.85 mg/mL in DMSO; ≥2.48 mg/mL in H2O with gentle warming and ultrasonic; ≥9.5 mg/mL in EtOH with ultrasonic
Chemical Name N-[[(5S)-3-(3-fluoro-4-morpholin-4-ylphenyl)-2-oxo-1,3-oxazolidin-5-yl]methyl]acetamide
Canonical SMILES CC(=O)NCC1CN(C(=O)O1)C2=CC(=C(C=C2)N3CCOCC3)F
Shipping Condition Ship with blue ice, or upon other requests.
General tips For obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. We do not recommend long-term storage for the solution, please use it up soon.

  Protocol  

Antibacterial test [1]:

Bacteria

E. coli UC6782

Preparation method

The solubility of this compound in DMSO is > 16.9 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months.

Reacting condition

0.01 ~ 1000 μM; 60 mins

Applications

Linezolid potently inhibited protein synthesis in E. coli UC6782, with the IC90 value of 30 μM. Linezolid was at least 2.5 times more potent than DuP-721 and about twice as potent as streptomycin.

 

 

 

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